The present invention relates to novel isocyanurates having at least two oxiranyl groups and the use of the same to treat malignant neoplasias and therapeutic compositions with a cytostatic action containing said isocyanurates having at least two oxiranyl groups.
It is known that a number of alkylating substances develop a cytostatic or cytotoxic effect. The best known compounds are derived from the so-called nitrogen mustards. Beyond that it is also known to use compounds containing at least two epoxy groups in the molecule as cancerostatic agents. Such compounds are, for instance, 4,4'-bis-(2,3-epoxypropyl)-di-piperidinyl-(1,1') and 1,2-15,16-diepoxy-4,7,10,13-tetraoxohexadecane. However, these diepoxide compounds did not provide substantial improvement in cytostatic treatment and they are hardly used. They are utilized only occasionally for the treatment of brain tumors. The wider applicability of the above-mentioned compounds is also prevented by their limited solubility.
The subject matter of commonly assigned copending U.S. Patent Application Ser. No. 95,229, filed Nov. 19, 1979, now abandoned in favor of continuation Ser. No. 257,893, filed Apr. 27, 1981, relates to therapeutic compositions having a cytostatic action which contain as the pharmacologically active ingredient triglycidyl isocyanurate (TGI) and/or such TGI derivatives where the hydrogen atom attached to the carbon in the 2 position of one or more of the glycidyl groups is replaced by an alkyl having from 1 to 4 carbon atoms. Compounds of this kind are characterized by the three nitrogen atoms of the isocyanuric acid ring being substituted by glycidyl groups containing epoxy groups, which can also be substituted in the 2 position with an alkyl having from 1 to 4 carbon atoms.
The subject matter of commonly assigned copending U.S. Patent Application Ser. No. 194,908, filed Oct. 7, 1980, likewise relates to cytostatically active pharmaceutical preparations which contain as the pharmacologically active ingredient isocyanurates corresponding to the formula ##STR3## where R is alkyl, aryl, aralkyl, alkaryl, cycloalkyl, where these radicals may optionally be unsaturated with/or substituted and glycidyl represents a group of the formula ##STR4## where R is hydrogen or an alkyl having from 1 to 4 carbon atoms.